1224713-71-6Relevant articles and documents
Synthesis and biological evaluation of stilbene derivatives coupled to NO donors as potential antidiabetic agents
Wang, Bing,Liu, Teng,Wu, Zhongyu,Zhang, Lei,Sun, Jie,Wang, Xiaojing
, p. 416 - 423 (2018)
The work is focused on the design of drugs that prevent and treat diabetes and its complications. A novel class of stilbene derivatives were prepared by coupling NO donors of alkyl nitrate and were fully characterised by NMR and other techniques. These compounds were tested in vitro activity, including α-glucosidase inhibitory activity, aldose reductase (AR) inhibitory activity and advanced glycation end products (AGEs) formation inhibitory activity. A class of modified compounds could play a significant effect for treatment of diabetic complications. Target compounds 3e and 7c offered a potential drug design concept for the development of therapeutic or preventive agents for diabetes and its complications.
Discovery of Novel Pterostilbene-Based Derivatives as Potent and Orally Active NLRP3 Inflammasome Inhibitors with Inflammatory Activity for Colitis
Chen, Liu Zeng,Diao, Liang Zhuo,Huang, Yan Shuang,Li, Qingshan,Liu, Ming Ming,Liu, Xin Hua,Ma, Duo,Ruan, Ban Feng,Wu, Jing,Zhang, Rui,Zhang, Xing Xing
, p. 13633 - 13657 (2021/09/28)
Studies have shown that the abnormal activation of the NLRP3 inflammasome is involved in a variety of inflammatory-based diseases. In this study, a high content screening model targeting the activation of inflammasome was first established and pterostilbene was discovered as the active scaffold. Based on this finding, total of 50 pterostilbene derivatives were then designed and synthesized. Among them, compound 47 was found to be the best one for inhibiting cell pyroptosis [inhibitory rate (IR) = 73.09% at 10 μM], showing low toxicity and high efficiency [against interleukin-1β (IL-1β): half-maximal inhibitory concentration (IC50) = 0.56 μM]. Further studies showed that compound 47 affected the assembly of the NLRP3 inflammasomes by targeting NLRP3. Thein vivobiological activity showed that this compound significantly alleviated dextran sodium sulfate (DSS)-induced colitis in mice. In general, our study provided a novel lead compound directly targeting the NLRP3 protein, which is worthy of further research and structural optimization.
NOVEL STILBENE ANALOGS
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Page/Page column 15, (2010/05/13)
The present invention relates to Stilbene derivatives of the general formula I or a pharmaceutically acceptable salt thereof have properties such as high water solubility, bioavailability and effective as carcinostatics.
